JP2016523226A5 - - Google Patents

Info

Publication number

JP2016523226A5

JP2016523226A5 JP2016517018A JP2016517018A JP2016523226A5 JP 2016523226 A5 JP2016523226 A5 JP 2016523226A5 JP 2016517018 A JP2016517018 A JP 2016517018A JP 2016517018 A JP2016517018 A JP 2016517018A JP 2016523226 A5 JP2016523226 A5 JP 2016523226A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

subject

composition according

hydroxyl

vitamin

Prior art date

2014-05-29

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

• Espacenet
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• 239000008194 pharmaceutical composition Substances 0.000 claims description 66
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 34
• 229930003316 Vitamin D Natural products 0.000 claims description 30
• 229940046008 Vitamin D Drugs 0.000 claims description 30
• 239000011710 vitamin D Substances 0.000 claims description 30
• 235000019166 vitamin D Nutrition 0.000 claims description 30
• 238000002512 chemotherapy Methods 0.000 claims description 27
• 150000002367 halogens Chemical class 0.000 claims description 26
• -1 vitamin D compound Chemical class 0.000 claims description 24
• 229910052736 halogen Inorganic materials 0.000 claims description 22
• 229910052739 hydrogen Inorganic materials 0.000 claims description 22
• 239000001257 hydrogen Substances 0.000 claims description 22
• 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims description 22
• 125000000217 alkyl group Chemical group 0.000 claims description 18
• 125000003545 alkoxy group Chemical group 0.000 claims description 16
• 201000004384 alopecia Diseases 0.000 claims description 14
• 231100000360 alopecia Toxicity 0.000 claims description 12
• 125000004093 cyano group Chemical group *C#N 0.000 claims description 12
• 230000000699 topical Effects 0.000 claims description 12
• 239000011647 vitamin D3 Substances 0.000 claims description 12
• 230000000977 initiatory Effects 0.000 claims description 11
• DNIAPMSPPWPWGF-UHFFFAOYSA-N propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 8
• 239000007921 spray Substances 0.000 claims description 8
• 238000002560 therapeutic procedure Methods 0.000 claims description 8
• GMRQFYUYWCNGIN-NKMMMXOESA-N (1R,3S,5Z)-5-{2-[(1R,3aS,4E,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-octahydro-1H-inden-4-ylidene]ethylidene}-4-methylidenecyclohexane-1,3-diol Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@@H](CCCC(C)(C)O)C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C GMRQFYUYWCNGIN-NKMMMXOESA-N 0.000 claims description 6
• 229960005084 CALCITRIOL Drugs 0.000 claims description 6
• 125000003342 alkenyl group Chemical group 0.000 claims description 6
• OYPRJOBELJOOCE-UHFFFAOYSA-N calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 6
• 229910052791 calcium Inorganic materials 0.000 claims description 6
• 239000011575 calcium Substances 0.000 claims description 6
• 201000011510 cancer Diseases 0.000 claims description 6
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 6
• 150000003710 vitamin D derivatives Chemical class 0.000 claims description 6
• BJYLYJCXYAMOFT-RRXOBRNQSA-N (1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-5-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCC(O)C(C)C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C BJYLYJCXYAMOFT-RRXOBRNQSA-N 0.000 claims description 4
• XXJWXESWEXIICW-UHFFFAOYSA-N 2-(2-Ethoxyethoxy)ethanol Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 claims description 4
• 125000001960 7 membered carbocyclic group Chemical group 0.000 claims description 4
• LWQQLNNNIPYSNX-UROSTWAQSA-N Calcipotriol Chemical compound C1([C@H](O)/C=C/[C@@H](C)[C@@H]2[C@]3(CCCC(/[C@@H]3CC2)=C\C=C\2C([C@@H](O)C[C@H](O)C/2)=C)C)CC1 LWQQLNNNIPYSNX-UROSTWAQSA-N 0.000 claims description 4
• 210000003780 Hair Follicle Anatomy 0.000 claims description 4
• 206010020583 Hypercalcaemia Diseases 0.000 claims description 4
• 210000004761 Scalp Anatomy 0.000 claims description 4
• QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 claims description 4
• 125000003118 aryl group Chemical group 0.000 claims description 4
• 229960004729 colecalciferol Drugs 0.000 claims description 4
• 239000003814 drug Substances 0.000 claims description 4
• 229940079593 drugs Drugs 0.000 claims description 4
• 125000001072 heteroaryl group Chemical group 0.000 claims description 4
• 230000000148 hypercalcaemia Effects 0.000 claims description 4
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 4
• 125000004665 trialkylsilyl group Chemical group 0.000 claims description 4
• QYSXJUFSXHHAJI-YRZJJWOYSA-N vitamin D3 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-YRZJJWOYSA-N 0.000 claims description 4
• 235000005282 vitamin D3 Nutrition 0.000 claims description 4
• 229940021056 vitamin D3 Drugs 0.000 claims description 4
• 150000003839 salts Chemical class 0.000 claims description 3
• 239000011780 sodium chloride Substances 0.000 claims description 3
• 206010002383 Angina pectoris Diseases 0.000 claims description 2
• 229940112871 Bisphosphonate drugs affecting bone structure and mineralization Drugs 0.000 claims description 2
• 206010006187 Breast cancer Diseases 0.000 claims description 2
• 206010007559 Cardiac failure congestive Diseases 0.000 claims description 2
• 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
• 229940030606 DIURETICS Drugs 0.000 claims description 2
• 206010014733 Endometrial cancer Diseases 0.000 claims description 2
• 210000000981 Epithelium Anatomy 0.000 claims description 2
• ZZUFCTLCJUWOSV-UHFFFAOYSA-N Furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 claims description 2
• 229960003883 Furosemide Drugs 0.000 claims description 2
• 208000000913 Kidney Calculi Diseases 0.000 claims description 2
• 208000010125 Myocardial Infarction Diseases 0.000 claims description 2
• 206010028980 Neoplasm Diseases 0.000 claims description 2
• 206010029148 Nephrolithiasis Diseases 0.000 claims description 2
• 210000000440 Neutrophils Anatomy 0.000 claims description 2
• 206010033128 Ovarian cancer Diseases 0.000 claims description 2
• 206010061920 Psychotic disease Diseases 0.000 claims description 2
• 206010038111 Recurrent cancer Diseases 0.000 claims description 2
• 206010039491 Sarcoma Diseases 0.000 claims description 2
• 210000002966 Serum Anatomy 0.000 claims description 2
• 206010044625 Trichorrhexis Diseases 0.000 claims description 2
• 125000000304 alkynyl group Chemical group 0.000 claims description 2
• 230000001396 anti-anti-diuretic Effects 0.000 claims description 2
• 150000004663 bisphosphonates Chemical class 0.000 claims description 2
• 235000020964 calcitriol Nutrition 0.000 claims description 2
• 239000011612 calcitriol Substances 0.000 claims description 2
• 230000003913 calcium metabolism Effects 0.000 claims description 2
• 229910052799 carbon Inorganic materials 0.000 claims description 2
• 125000004432 carbon atoms Chemical group C* 0.000 claims description 2
• 210000004027 cells Anatomy 0.000 claims description 2
• 201000010881 cervical cancer Diseases 0.000 claims description 2
• 201000006233 congestive heart failure Diseases 0.000 claims description 2
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
• 239000002934 diuretic Substances 0.000 claims description 2
• 230000002500 effect on skin Effects 0.000 claims description 2
• 201000001342 fallopian tube cancer Diseases 0.000 claims description 2
• 230000003676 hair loss Effects 0.000 claims description 2
• 125000000623 heterocyclic group Chemical group 0.000 claims description 2
• 230000004987 nonapoptotic Effects 0.000 claims description 2
• 201000008968 osteosarcoma Diseases 0.000 claims description 2
• 125000004043 oxo group Chemical group O=* 0.000 claims description 2
• 125000000547 substituted alkyl group Chemical group 0.000 claims description 2
• 239000003451 thiazide diuretic agent Substances 0.000 claims description 2
• 231100000419 toxicity Toxicity 0.000 claims description 2
• 230000001988 toxicity Effects 0.000 claims description 2
• 230000003778 catagen phase Effects 0.000 description 1